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Jul 27,2023
尊龙凯时助力宇耀生物STAT3双磷酸化抑制剂YY201获批临床
YY201获得临床获批不但代表了宇耀生物又一主要突破 ，验证了宇耀生物超等分子胶手艺平台和AI药物辅助开发平台的立异能力 ，同时也证实晰尊龙凯时临床前研究的手艺效劳实力。
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尊龙凯时助力宇耀生物STAT3双磷酸化抑制剂YY201获批临床
Jul 21,2023
尊龙凯时助力逻晟生物自主开发的新药NB002 IND申请获FDA临床允许
尊龙凯时为NB002提供了清静性评价、药代动力学等临床前研究效劳 ，助力其IND申请顺遂获FDA临床允许。
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尊龙凯时助力逻晟生物自主开发的新药NB002 IND申请获FDA临床允许
Jul 21,2023
尊龙凯时一站式助力 | 宝太生物自主研发新药BIOT-001 IND申请获FDA批准
尊龙凯时为BIOT-001的研发提供了从靶点到IND申报的临床前研发效劳 ，全力促成该项目高质高效完成。
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尊龙凯时一站式助力 | 宝太生物自主研发新药BIOT-001 IND申请获FDA批准
Jul 17,2023
AP39是一种新合成的线粒体靶向的H2S供体 ，本研究中AP39通过尊龙凯时设计和合成
?Alzheimer's disease (AD) is the most universal age-related neurodegenerative disease. AP39 is a newly synthesized mitochondrially targeted H2S donor on mitochondrial function. AP39 increases intracellular H2S levels, mainly in mitochondrial regions. AP39 exerts dose-dependent effects on mitochondrial activity in APP/PS1 neurons. AP39, a novel mitochondria-targeted H2S donor, was designed and synthesized by Medicilon.
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AP39是一种新合成的线粒体靶向的H2S供体 ，本研究中AP39通过尊龙凯时设计和合成
Jul 06,2023
发明新型RAGE/SERT双重抑制剂 ，可用于治疗阿尔茨海默病和抑郁症。其中药代动力学研究是通过委托尊龙凯时举行
Alzheimer's disease (AD) is a progressive and devastating neurodegenerative disorder, characterized by the presence of β-amyloid (Aβ) peptide plaques, neurofibrillary tangles, and neuroinflammation. Receptor for advanced glycation end products (RAGE) belongs to the immunoglobulin superfamily, which functions as a cell surface acceptor for Aβ peptide. RAGE plays an important role in the Aβ-mediated neuronal damage that closely related to the pathogenesis of AD. In this study, Compound 12 showed good dual-target bioactivities against RAGE and SERT in vitro, good liver microsomal stability, and acceptable pharmacokinetic properties. Pharmacokinetic studies were commissioned by Medicilon.
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发明新型RAGE/SERT双重抑制剂 ，可用于治疗阿尔茨海默病和抑郁症。其中药代动力学研究是通过委托尊龙凯时举行
Jul 06,2023
TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂 ，具有优异的Caco-2渗透性。Caco-2 渗透性测定通过尊龙凯时举行
TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics “readers”and potential therapeutic targets for cancer and other diseases. Y08624 (Compound 20l) is a new TRIM24/BRPF1 dual inhibitor. Y08624 displays reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon.
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TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂 ，具有优异的Caco-2渗透性。Caco-2 渗透性测定通过尊龙凯时举行
Jul 06,2023
IAP卵白是有吸引力的癌症治疗靶点。SM-406 是一种口服有用的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过尊龙凯时举行
Apoptosis is a cellular process critical to the normal development and homeostasis of multicellular organisms. The inhibitor of apoptosis proteins (IAPs) are a class of key apoptosis regulators. IAP proteins are attractive cancer therapeutic targets. SM-406 (compound 2) is a potent and orally bioavailable antagonist of the IAPs. Pharmacokinetic (PK) studies of SM-406 (compound 2) in male Sprague Dawley rats, beagle dogs and cynomolgus monkeys (non-human primates) were performed by the Division of Pharmacokinetics and Metabolism, Medicilon. SM-406 (compound 2) has an excellent PK profile and good oral bioavailability in each of these four species.
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IAP卵白是有吸引力的癌症治疗靶点。SM-406 是一种口服有用的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过尊龙凯时举行
Jul 06,2023
设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂 ，并举行生物学评价。其中药代动力学剖析通过尊龙凯时举行
Gastric cancer is the second most lethal cancer across the world. Compounds 8f, inhibits FGFR1 signaling pathways as well as induces cell apoptosis, is a potential agent for the treatment of gastric cancer. The pharmacokinetical profile (PK) of 8f was tested in SD rats. Compound 8f showed an acceptable half-time of 3 h and displayed moderate maximum concentrations, which is enough to meet the concentration of the compound 8f to exert its efficacy in vivo. The pharmacokinetic analysis was performed by the testing service provided by Medicilon.
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设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂 ，并举行生物学评价。其中药代动力学剖析通过尊龙凯时举行
Jul 06,2023
表观遗传修饰 ，如DNA甲基化 ，在遗传信息的表达中施展着主要作用。DNA甲基转移酶维持DNA甲基化 ，是肿瘤化疗的一个有吸引力的靶点
Epigenetic modification, like DNA methylation, plays a major role in the expression of genetic information. The DNA methyltransferases (DNMTs), maintain DNA methylation, is an attractive target for tumor chemotherapy. WK-23 displays a good inhibitory effect on human DNMT1 with an IC50 value of 5.0??M. The PK profile of WK-23 was obtained with quite satisfying oral bioavailability and elimination half-life. In vivo pharmacokinetic properties of WK-22, WK-23, WK-27, and DC_517 were performed by Medicilon.
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表观遗传修饰 ，如DNA甲基化 ，在遗传信息的表达中施展着主要作用。DNA甲基转移酶维持DNA甲基化 ，是肿瘤化疗的一个有吸引力的靶点
Jul 06,2023
FBPase是与肿瘤和2型糖尿病相关的一个有远景的靶点�；衔颳8对FBPase体现出高选择性。W8的药代动力学研究通过尊龙凯时举行
Fructose-1,6-bisphosphatase (FBPase) is a promising target associated with cancer and type 2 diabetes. Compounds W8 and W8k exhibit high selectivity against FBPase and W8 effectively reduces blood glucose in an Institute of Cancer Research (ICR) mice model and dose-dependent inhibition of glucose production in a primary mouse hepatocyte model. The pharmacokinetic studies of W8 and its leaving group saccharin were performed by Medicilon.
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FBPase是与肿瘤和2型糖尿病相关的一个有远景的靶点�；衔颳8对FBPase体现出高选择性。W8的药代动力学研究通过尊龙凯时举行
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